| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
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| ln Vitro |
ZAP-70 (pIC50=4.7), LCK (pIC50=5.3), LYN (pIC50=5.4), JAK1/2/3 (pIC50=5.8/5.8/5.7), Aurora B (pIC50=4.8), hWB (pIC50=6.6), and hERG (pIC50=4.7) are all inhibited by GSK143 (compound 20)[1]. In CLL cells, GSK143 (10–10,000 nM; every 24 hours for three days) exhibits an IC50 of 323 nM. Early signaling processes, such as SYK phosphorylation and calcium flow, are abrogated by GSK 143 (1 μM; 30 mins)[2]. In bone marrow-derived macrophages, GSK143 (0.1–10 μM) decreases cytokine expression in a concentration-dependent manner lasting 30 minutes[3].
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| ln Vivo |
In the intestinal muscularis, GSK143 (0.1–10 mg/kg; orally; 1.5 hours) decreases inflammation and inhibits the recruitment of immune cells[3]. The cutaneous reverse passive Arthus reaction is reduced by GSK143 (3, 10, 30, 100 mg/kg; oral; one hour before ovalbumin challenge) in a dose-dependent manner by around 50% and 70% at 10 mg/kg and 30 mg/kg, respectively[2]. GSK143 in rats has a T1/2 of 4.2 hours, a low clearance of 16 mL/min/kg, a moderate bioavailability of 30%, and a Vss of 4.1 L/kg (iv of 1 mg/kg; po of 3 mg/kg)[1].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Chronic lymphocytic leukemia (CLL) cells Tested Concentrations: 10, 100, 1000, 10000 nM Incubation Duration: Every 24 h for 3 days Experimental Results: Had an IC50 of 323 nM. |
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| Animal Protocol |
Animal/Disease Models: Wild type C57NL/BL6 mice, 10-12 weeks old[3]
Doses: 0.1, 1, 3, 10 mg/kg Route of Administration: po (oral gavage) 1.5 hrs (hours) before intestinal manipulation (IM) Experimental Results: decreased inflammation and prevented recruitment of immune cells in the intestinal muscularis. Animal/Disease Models: Male CD rats (175-200 g)[1] Doses: 1 mg/kg of iv; 3 mg/kg of po (pharmacokinetic/PK Analysis) Route of Administration: IV or PO Experimental Results: Had a T1/2 of 4.2 hrs (hours), low clearance (16 mL/min/kg), moderate bioavailability of 30% and a Vss of 4.1 L/kg. |
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| References |
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| Additional Infomation |
See also: Gsk143 (annotation moved to).
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| Molecular Formula |
C17H22N6O2
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|---|---|
| Molecular Weight |
342.39558
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| Exact Mass |
342.18
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| CAS # |
1240390-27-5
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| Related CAS # |
GSK143 dihydrochloride;2341796-81-2
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| PubChem CID |
46865656
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.702
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
443
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1=CC=C(NC2=NC(N[C@@H]3CCOC[C@@H]3N)=NC=C2C(N)=O)C=C1
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| InChi Key |
KBPYMFSSFLOJPH-UONOGXRCSA-N
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| InChi Code |
InChI=1S/C17H22N6O2/c1-10-2-4-11(5-3-10)21-16-12(15(19)24)8-20-17(23-16)22-14-6-7-25-9-13(14)18/h2-5,8,13-14H,6-7,9,18H2,1H3,(H2,19,24)(H2,20,21,22,23)/t13-,14+/m0/s1
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| Chemical Name |
2-[[(3R,4R)-3-aminooxan-4-yl]amino]-4-(4-methylanilino)pyrimidine-5-carboxamide
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| Synonyms |
GSK-143 GSK 143 GSK143
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9206 mL | 14.6028 mL | 29.2056 mL | |
| 5 mM | 0.5841 mL | 2.9206 mL | 5.8411 mL | |
| 10 mM | 0.2921 mL | 1.4603 mL | 2.9206 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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